The physical form of an active pharmaceutical ingredient (API) has great significance from the perspectives of drug product performance, intellectual property protection, and regulatory compliance, etc.1-3 The quality of the lead candidates can be favorably impacted by early consideration of “developability” criteria along with efficacy and safety studies.4,5 For instance, if non-developable forms, such as oils, amorphous materials, and some solvates, etc., were elevated, lots of downstream development difficulties would emerge. These difficulties could severely delay the formulation development process as well as other project-relevant activities. In addition, on the discovery side, efficacy and safety studies might not be conducted because of the challenges caused by those form issues.
Currently various API-sparing experimental strategies are proposed and practiced to rapidly and effectively evaluate the polymorphism and crystallization tendency of the compounds advancing from discovery into early development Although both experimental and theoretical strategies have been focused in the area of crystallization and polymorphism,1,7-10; however there are severe limitations associated with the existing methods:
First of all, computational methods are far from practical application because they are very expensive, time-consuming, and specially-trained talents are required. More importantly, the predictive power on polymorphism is not satisfying so far.11 
As for experimental methods, high-throughput form screening is not quite satisfying, which is often attributed to the consensus that polymorph screening is partially both science and art. In fact, the fundamental reason is lack of fundamental understanding of polymorphism. In addition, more comprehensive polymorph screening on discovery compounds before elevation is not realistic because of its cost- and time-ineffectiveness at this stage.
Therefore, a process for risk assessment of discovery compounds is needed before their elevation for development, as this would greatly facilitate the identification of those drug candidates with the most promising developability. The present invention provides such a process.
Sherry L. Morissette et al., Advanced Drug Delivery Reviews 56 (2004) 275-300, reviews and highlights the opportunities and challenges of high throughput crystallization technologies as they apply to pharmaceutical research and development.
Alejandro J. Alvarez et al., Crystal Growth and Design, 2009, Vol. 9, No. 9, 4181-4188, compares the polymorph screening studies of various compounds using a semi-automated apparatus with a high-throughput method.